Synthesis of diphenoxyadamantane alkylamines with pharmacological interest.

Markos-Orestis Georgiadis; Violeta Kourbeli; Vaya Ioannidou; Evangelos Karakitsios; Ioannis Papanastasiou; Andrew Tsotinis; Dimitri Komiotis; Anthony Vocat; Stewart T Cole; Martin C Taylor ORCID logo; +1 more... John M Kelly ORCID logo; (2019) Synthesis of diphenoxyadamantane alkylamines with pharmacological interest. Bioorganic & medicinal chemistry letters, 29 (11). pp. 1278-1281. ISSN 0960-894X DOI: 10.1016/j.bmcl.2019.04.010
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In this work, the synthesis and the pharmacological evaluation of diphenoxyadamantane alkylamines Ia-f and IIa-f is described. The new diphenoxy-substituted adamantanes share structural features present in trypanocidal and antitubercular agents. 1-Methylpiperazine derivative Ia is the most potent against T. brucei compound, whilst its hexylamine congener IIf exhibits a significant antimycobacterial activity.


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